2. Cell Cycle/DNA Damage
  3. CDK
  4. AG-024104

AG-024104 is a CDK inhibitor with Ki values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development.

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AG-024104

AG-024104 Chemical Structure

CAS No. : 750575-23-6

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AG-024104 Related Antibodies

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Description

AG-024104 is a CDK inhibitor with Ki values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development[1].

In Vitro

AG-024104 potently inhibits purified CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD enzymes with Ki values of 2.3 nM, 1.8 nM, and 0.67 nM, respectively[1].
AG-024104 (4 days) inhibits HCT-116 colorectal carcinoma cell growth with an IC50 of 51 nM[1].
AG-024104 (24 h) induces cytotoxicity in human PBMCs and monkey PBLs with TC50 values of 7.2 μM and 4.0 μM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AG-024104 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT-116 colorectal carcinoma cells
Concentration: concentrations to achieve 50% growth inhibition (IC50 determination)
Incubation Time: 4 days
Result: Inhibited HCT-116 cell growth with an IC50 of 51 nM.
Parmacokinetics
Species Dose Route AUC0-24 T1/2
Rat[1] 10 mg/kg i.v. 2.7 μg·h/mL 1.4 h
In Vivo

AG-024104 (10 mg/kg; i.v.; single bolus injection over 2-3 min) does not induce significant acute suppression of peripheral white blood cell counts in male Sprague Dawley rats, with counts remaining at ~93% of pre-treatment levels 24 hours post-dose[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague Dawley (male, ~10 weeks old)[1]
Dosage: 10 mg/kg
Administration: i.v.; single bolus injection over 2-3 min
Result: Remained at ~93% of pre-treatment levels 24 hours post-dose.
Molecular Weight

566.64

Formula

C24H28F2N6O4S2
CAS No.
SMILES

O=C(C=1SC(=NC1N)NC2CCN(CC2)S(=O)(=O)C3=CN=C(OCCN(C)C)C=C3)C=4C(F)=CC=CC4F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AG-024104 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AG-024104750575-23-6AG024104AG 024104CDKCyclin dependent kinaselymphocytesCDK4/cyclinDCDK1/cyclinBnude mouse xenograft modelsHCT-116 colorectal carcinoma cellmonkey peripheral blood mononuclear cellsSprague Dawley ratscolorectal carcinoma cellsCDK2/cyclinAhuman peripheral blood mononuclear cellsInhibitorinhibitorinhibit

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